From Wikipedia, the free encyclopedia
Chemical structure of tirbanibulin Src inhibitor is a class of inhibitors[
jargon ] that targets the
Src kinase family of
tyrosine kinase , which is transcribed by the
Src
proto-oncogene (short for "
sarcoma gene") that potentially induce malignant transformations of certain cells. Because of the crucial position of the
Src kinase in cells, Src inhibitors are potential antineoplastic agents for e.g.
pancreatic cancer ,
breast cancer and
stomach cancer
[1]
Examples
Tirbanibulin is an oral src inhibitor and the first clinical inhibitor with GI50 of 9–60 nM in cancer cell lines.
[2]
Bosutinib has been developed for the treatment of chronic myelogenous
leukemia by
Pfizer .
Saracatinib , the first Src inhibitor to show inhibition of the Src pathway in human tumor tissue, has anti-tumor activity alone or in combination with chemotherapeutic agents.
[3]
Chemical structure of PP1
References
^
a
b Rivera-Torres J, José ES (2019).
"Src Tyrosine Kinase Inhibitors: New Perspectives on Their Immune, Antiviral, and Senotherapeutic Potential" .
Frontiers in Pharmacology . 10 : 1011.
doi :
10.3389/fphar.2019.01011 .
PMC
6759511 .
PMID
31619990 .
^ Antonarakis ES, Heath EI, Posadas EM, Yu EY, et al. (Apr 2013).
"A phase 2 study of KX2-391, an oral inhibitor of Src kinase and tubulin polymerization, in men with bone-metastatic castration-resistant prostate cancer" . Cancer Chemother Pharmacol . 71 (4): 883–892.
doi :
10.1007/s00280-013-2079-z .
PMC
3609871 .
PMID
23314737 .
^ Nam HJ, et al. (2013).
"Antitumor activity of saracatinib (AZD0530), a c-Src/Abl kinase inhibitor, alone or in combination with chemotherapeutic agents in gastric cancer" . Mol. Cancer Ther . 12 (1): 16–26.
doi :
10.1158/1535-7163.MCT-12-0109 .
PMID
23144237 .
^
"PP1 is a potent and selective Src inhibitor for Lck/Fyn" .
^
"biological activity of PP2 in selleck chemicals" . Selleck Texas.
^ Chan CM, Jing X, Pike LA, Zhou Q, Schweppe RE (2012).
"Targeted inhibition of Src kinase with dasatinib blocks thyroid cancer growth and metastasis" .
Clinical Cancer Research . 18 (13): 3580–91.
doi :
10.1158/1078-0432.CCR-11-3359 .
PMC
3931551 .
PMID
22586301 .